Immuno-Grade S1P2 Receptor Antibodies
The sphingosine-1-phosphate receptor 2 (S1P2 receptor) is a G protein-coupled receptor (GPCR) that mediates the cellular effects of sphingosine-1-phosphate (S1P), a bioactive lipid involved in vascular homeostasis, immune regulation, and cell migration. S1P2 receptor expression is regulated by developmental cues, inflammatory mediators, and tissue-specific transcriptional programs, with high expression in the vascular system, liver, inner ear, and certain immune cells. Upon activation, the receptor primarily couples to G12/13, Gq, and Gi proteins, leading to Rho activation, calcium signaling, and modulation of MAPK and PI3K pathways. In contrast to other S1P receptors, S1P2 often inhibits cell migration while promoting cytoskeletal rearrangement and barrier function. Dysregulated S1P2 signaling has been implicated in fibrosis, atherosclerosis, cancer progression, hearing disorders, and inflammatory diseases. Receptor activity is further regulated by ligand availability, receptor internalization, and feedback mechanisms that influence downstream signaling. Although several selective S1P2 antagonists, such as JTE-013, are widely used in experimental research, no S1P2-specific drugs have yet been approved for clinical use. S1P2 receptor desensitization, β-arrestin recruitment and internalization are regulated by phosphorylation of carboxyl-terminal serine330/serine331 (pS330/pS331-S1P2) and threonine342/serine343 (pT342/pS343-S1P2). This nomenclature refers to the human S1P2 receptor. This phosphorylation motif is highly conserved across species and is identical mice, rats and humans. For more information on S1P2 pharmacology please refer to the IUPHAR database. For further reading refer to:
Chun J, Hla T, Lynch KR, Spiegel S, Moolenaar WH. International Union of Basic and Clinical Pharmacology. LXXVIII. Lysophospholipid receptor nomenclature. Pharmacol Rev. 2010 Dec;62(4):579-87. doi: 10.1124/pr.110.003111. PMID: 21079037; PMCID: PMC2993255.
Kihara Y, Maceyka M, Spiegel S, Chun J. Lysophospholipid receptor nomenclature review: IUPHAR Review 8. Br J Pharmacol. 2014 Aug;171(15):3575-94. doi: 10.1111/bph.12678. Epub 2014 Jul 12. PMID: 24602016; PMCID: PMC4128058.
Blaho V, Chun J, Herr D, Jones D, Jonnalagadda D, Kihara Y. Lysophospholipid (S1P) receptors in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1).